专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

WO1997049704A1 N-[4-(HETEROARYLMETHYL)PHENYL]-HETEROARYLAMINES 审中-公开
标题翻译： N- [4-（杂芳基）苯基] -HETEROARYLAMINES
公开(公告)号：WO1997049704A1
公开(公告)日：1997-12-31
申请号：PCT/EP1997003248
申请日：1997-06-19
申请人： JANSSEN PHARMACEUTICA N.V. , VENET, Marc, Gaston , MABIRE, Dominique, Jean-Pierre , LACRAMPE, Jean, Fernand, Armand , SANZ, Gérard, Charles
发明人： JANSSEN PHARMACEUTICA N.V.
IPC分类号： C07D417/12
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D403/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D487/04 , C07D513/04
摘要： The present invention is concerned with compounds of formula (I), the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R is hydrogen, hydroxy, C1-6alkyl or aryl; R is hydrogen; optionally substituted C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl, optionally substituted pyrrolidinyl or aryl; R is hydrogen, optionally substituted C1-6alkyl or aryl; Het is an optionally substituted unsaturated heterocycle selected from imidazolyl, triazolyl, tetrazolyl and pyridinyl; formula (1) is an optionally substituted unsaturated mono- or bicyclic heterocycle; and aryl is optionally substituted phenyl. The present invention also relates to processes for their preparation and compositions comprising said new compounds, as well as their use as a medicine.
摘要翻译：本发明涉及式（I）化合物，N-氧化物，其药学上可接受的加成盐和立体化学异构形式，其中R 1是氢，羟基，C 1-6烷基或芳基; R 2是氢; 任选取代的C 1-12烷基; 3-7环烷基; C 2-8烯基，任选取代的吡咯烷基或芳基; R 3是氢，任选取代的C 1-6烷基或芳基; Het是选自咪唑基，三唑基，四唑基和吡啶基的任选取代的不饱和杂环; 式（1）是任选取代的不饱和单环或双环杂环; 并且芳基是任选取代的苯基。本发明还涉及其制备方法和包含所述新化合物的组合物，以及它们作为药物的用途。

2. 发明申请

WO1996020200A1 6-[TRIAZOLYL[3-(TRIFLUOROMETHYL)PHENYL]METHYL]-2-QUINOLINONES AND -QUINOLINETHIONES 审中-公开
标题翻译： 6- [三唑并[3-（三氟甲基）苯基]甲基] -2-喹啉酮和二氢化茚
公开(公告)号：WO1996020200A1
公开(公告)日：1996-07-04
申请号：PCT/EP1995005173
申请日：1995-12-21
申请人： JANSSEN PHARMACEUTICA N.V. , VENET, Marc, Gaston , MABIRE, Dominique, Jean-Pierre , SANZ, Gérard, Charles
发明人： JANSSEN PHARMACEUTICA N.V.
IPC分类号： C07D521/00
CPC分类号： C07D249/08 , C07D231/12 , C07D233/56
摘要： This invention is concerned with the compounds of formula (I), the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein R is hydrogen, amino or C1-4alkyl; R is hydrogen, halo or C1-4alkyl; R is hydrogen, halo or C1-4alkyl; Y is O or S, and -X = X - is a bivalent radical having the formula: -N = CH- (a-1) or -CH = N- (a-2); compositions containing the same, and processes of preparing these compounds. It further relates to their use as a medicine, in particular their use as a medicine to treat keratinization disorders.
摘要翻译：本发明涉及式（I）化合物，其药学上可接受的酸加成盐及其立体化学异构形式，其中R 1是氢，氨基或C 1-4烷基; R 2是氢，卤素或C 1-4烷基; R 3是氢，卤素或C 1-4烷基; Y是O或S，-X 1 = X 2 - 是具有下式的二价基团：-N = CH-（a-1）或-CH = N-（a-2）; 含有它们的组合物，以及制备这些化合物的方法。它还涉及它们作为药物的用途，特别是它们作为治疗角质化障碍的药物的用途。

3. 发明申请

WO1997021701A1 FARNESYL PROTEIN TRANSFERASE INHIBITING (IMIDAZOL-5-YL)METHYL-2-QUINOLINONE DERIVATIVES 审中-公开
标题翻译：蛋氨酸转运酶抑制剂（咪咪唑-5-基）甲基-2-喹啉酮衍生物
公开(公告)号：WO1997021701A1
公开(公告)日：1997-06-19
申请号：PCT/EP1996004515
申请日：1996-10-16
申请人： JANSSEN PHARMACEUTICA N.V. , VENET, Marc, Gaston , ANGIBAUD, Patrick, René , MULLER, Philippe , SANZ, Gérard, Charles
发明人： JANSSEN PHARMACEUTICA N.V.
IPC分类号： C07D401/06
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D401/06 , C07D401/14 , C07D405/14 , C07D407/14 , C07D413/14 , Y02P20/55
摘要： This invention comprises the novel compounds of formula (I), wherein the dotted line represents an optional bond; X is oxygen or sulfur; R is hydrogen, C1-12alkyl, Ar , Ar C1-6alkyl, quinolinylC1-6alkyl, pyridylC1-6alkyl, hydroxyC1-6alkyl, C1-6alkyloxyC1-6alkyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, aminoC1-6alkyl, or a radical of formula -Alk -C(=O)-R , -Alk -S(O)-R or -Alk -S(O)2-R ; R , R and R each independently are hydrogen, hydroxy, halo, cyano, C1-6alkyl, C1-6alkyloxy, hydroxyC1-6alkyloxy, C1-6alkyloxyC1-6alkyloxy, aminoC1-6alkyloxy, mono- or di(C1-6alkyl)aminoC1-6alkyloxy, Ar , Ar C1-6alkyl, Ar oxy, Ar C1-6alkyloxy, hydroxycarbonyl, C1-6alkyloxycarbonyl, trihalomethyl, trihalomethoxy, C2-6alkenyl; R and R each independently are hydrogen, halo, Ar , C1-6alkyl, hydroxyC1-6alkyl, C1-6alkyloxyC1-6alkyl, C1-6alkyloxy, C1-6alkylthio, amino, hydroxycarbonyl, C1-6alkyloxycarbonyl, C1-6alkylS(O)C1-6alkyl or C1-6alkylS(O)2C1-6alkyl; R and R each independently are hydrogen, halo, cyano, C1-6alkyl, 4,4-dimethyl-oxazolyl, C1-6alkyloxy or Ar oxy; R is hydrogen, C1-6alkyl, cyano, hydroxycarbonyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonylC1-6alkyl, cyanoC1-6alkyl, C1-6alkyloxycarbonylC1-6alkyl, carboxyC1-6alkyl, hydroxyC1-6alkyl, aminoC1-6alkyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, imidazolyl, haloC1-6alkyl, C1-6alkyloxyC1-6alkyl, aminocarbonylC1-6alkyl, or a radical of formula -O-R , -S-R , -N-R R ; R is hydrogen, halo, cyano, C1-6alkyl, C1-6alkyloxycarbonyl, Ar ; R is hydrogen, C1-6alkyl, C1-6alkyloxy or halo; R is hydrogen or C1-6alkyl; having farnesyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.
摘要翻译：本发明包括式（I）的新化合物，其中虚线表示任选的键; X是氧或硫; R 1是氢，C 1-12烷基，Ar 1，Ar 2 C 1-6烷基，喹啉基C 1-6烷基，吡啶基C 1-6烷基，羟基C 1-6烷基，C 1-6烷氧基C 1-6烷基，单或二（C 1-6烷基）氨基C 1-6烷基，氨基C 1-6烷基或式-Ak 1 -C（= O）-R 9，-AlK 1 -S（O）-R 9或-Alk 1> -S（O）2-R <9>; R 2，R 3和R 16各自独立地是氢，羟基，卤素，氰基，C 1-6烷基，C 1-6烷氧基，羟基C 1-6烷氧基，C 1-6烷氧基C 1-6烷氧基，氨基C 1-6烷氧基，单或二（C 1-6烷基）氨基C 1-6烷氧基，Ar 1，Ar 2 C 1-6烷基，Ar 2氧基，Ar 2 C 1-6烷氧基，羟基羰基，C 1-6烷氧基羰基，三卤甲基，三卤甲氧基，C 2-6烯基 ; R 4和R 5各自独立地为氢，卤素，Ar 1，C 1-6烷基，羟基C 1-6烷基，C 1-6烷氧基C 1-6烷基，C 1-6烷氧基，C 1-6烷硫基，氨基，羟基羰基，C 1-6烷氧基羰基，C 1-6烷基S（O）C 1-6烷基或C 1-6烷基S（O）2 C 1-6烷基; R 6和R 7各自独立地为氢，卤素，氰基，C 1-6烷基，4,4-二甲基 - 恶唑基，C 1-6烷氧基或Ar 2氧基; R 8是氢，C 1-6烷基，氰基，羟基羰基，C 1-6烷氧基羰基，C 1-6烷基羰基C 1-6烷基，氰基C 1-6烷基，C 1-6烷氧基羰基C 1-6烷基，羧基C 1-6烷基，羟基C 1-6烷基，氨基C 1-6烷基，二（C 1-6烷基）氨基C 1-6烷基，咪唑基，卤代C 1-6烷基，C 1-6烷氧基C 1-6烷基，氨基羰基C 1-6烷基或式-OR 10，-SR 10，-NR 11 R 12>; R 17是氢，卤素，氰基，C 1-6烷基，C 1-6烷氧基羰基，Ar 1; R 18是氢，C 1-6烷基，C 1-6烷氧基或卤素; R 19是氢或C 1-6烷基; 具有法呢基转移酶抑制活性; 其制剂，含有它们的组合物及其作为药物的用途。

4. 发明申请

WO1997016443A1 FARNESYL TRANSFERASE INHIBITING 2-QUINOLONE DERIVATIVES 审中-公开
标题翻译：呋喃酮转移抑制2-喹啉酮衍生物
公开(公告)号：WO1997016443A1
公开(公告)日：1997-05-09
申请号：PCT/EP1996004661
申请日：1996-10-25
申请人： JANSSEN PHARMACEUTICA N.V. , END, David, William , VENET, Marc, Gaston , ANGIBAUD, Patrick, René , SANZ, Gérard, Charles
发明人： JANSSEN PHARMACEUTICA N.V.
IPC分类号： C07D401/06
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D401/06
摘要： The present invention is concerned with compounds of formula (I), the stereoisomeric forms thereof and the pharmaceutically acceptable acid or base addition salts thereof, wherein the dotted line represents an optional bond; X is oxygen or sulfur; R is hydrogen, C1-12alkyl, Ar , Ar C1-6alkyl, quinolinylC1-6alkyl, pyridylC1-6alkyl, hydroxyC1-6alkyl, C1-6alkyloxyC1-6alkyl, mono- or di(C1-6alkyl)-aminoC1-6alkyl, aminoC1-6alkyl, or a radical of formula -Alk -C(=O)-R , -Alk -S(O)-R or -Alk -S(O)2-R ; R and R each independently are hydrogen, hydroxy, halo, cyano, C1-6alkyl, C1-6alkyloxy, hydroxyC1-6alkyloxy, C1-6alkyloxy-C1-6alkyloxy, aminoC1-6alkyloxy, mono- or di(C1-6alkyl)aminoC1-6alkyloxy, Ar , Ar C1-6alkyl, Ar oxy, Ar C1-6alkyloxy, hydroxycarbonyl, C1-6alkyloxycarbonyl, trihalomethyl, trihalomethoxy, C2-6alkenyl; or when on adjacent positions R and R taken together may form a bivalent radical; R and R each independently are hydrogen, Ar , C1-6alkyl, C1-6alkyloxy-C1-6alkyl, C1-6alkyloxy, C1-6alkylthio, amino, hydroxycarbonyl, C1-6alkyloxycarbonyl, C1-6alkylS(O)C1-6alkyl or C1-6alkylS(O)2-C1-6alkyl; R and R each independently are hydrogen, halo, cyano, C1-6alkyl, C1-6alkyloxy or Ar oxy; R is hydrogen, C1-6alkyl, cyano, hydroxycarbonyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonylC1-6alkyl, cyanoC1-6alkyl, C1-6alkyloxycarbonylC1-6alkyl, hydroxycarbonyl-C1-6alkyl, hydroxyC1-6alkyl, aminoC1-6alkyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, haloC1-6alkyl, C1-6alkyloxy-C1-6alkyl, aminocarbonylC1-6alkyl, Ar , Ar C1-6alkyloxyC1-6alkyl, C1-6alkylthioC1-6alkyl; R is hydrogen, C1-6alkyl or halo; R is hydrogen or C1-6alkyl; having farnesyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.
摘要翻译：本发明涉及式（I）化合物，其立体异构形式及其药学上可接受的酸或碱加成盐，其中虚线表示任选的键; X是氧或硫; R 1是氢，C 1-12烷基，Ar 1，Ar 2 C 1-6烷基，喹啉基C 1-6烷基，吡啶基C 1-6烷基，羟基C 1-6烷基，C 1-6烷氧基C 1-6烷基，单或二（C 1-6烷基） - 氨基C 1-6烷基，氨基C 1-6烷基或式-Ak 1 -C（= O）-R 9，-AlK 1 -S（O）-R 9或-Alk <1> -S（O）2-R <9>; R 2和R 3各自独立地是氢，羟基，卤素，氰基，C 1-6烷基，C 1-6烷氧基，羟基C 1-6烷氧基，C 1-6烷氧基-C 1-6烷氧基，氨基C 1-6烷氧基，一或二（C 1 1-6烷基）氨基C 1-6烷氧基，Ar 1，Ar 2 C 1-6烷基，Ar 2氧基，Ar 2 C 1-6烷氧基，羟基羰基，C 1-6烷氧基羰基，三卤甲基，三卤甲氧基，C 2-6烯基; 或者当相邻位置R 2和R 3一起形成二价基团时; R 4和R 5各自独立地为氢，Ar 1，C 1-6烷基，C 1-6烷氧基-C 1-6烷基，C 1-6烷氧基，C 1-6烷硫基，氨基，羟基羰基，C 1-6烷氧基羰基，C 1-6烷基（O）C 1-6烷基或C 1-6烷基S（O）2 -C 1-6烷基; R 6和R 7各自独立地为氢，卤素，氰基，C 1-6烷基，C 1-6烷氧基或Ar 2氧基; R 8是氢，C 1-6烷基，氰基，羟基羰基，C 1-6烷氧基羰基，C 1-6烷基羰基C 1-6烷基，氰基C 1-6烷基，C 1-6烷氧基羰基C 1-6烷基，羟基羰基-C 1-6烷基，羟基C 1-6烷基，氨基C 1-6烷基，单 - 或二（C 1-6烷基）氨基C 1-6烷基，卤代C 1-6烷基，C 1-6烷氧基-C 1-6烷基，氨基羰基C 1-6烷基，Ar 1，Ar 2 C 1-6烷氧基C 1-6烷基，C 1-6烷硫基C 1-6烷基; R 10是氢，C 1-6烷基或卤素; R 11是氢或C 1-6烷基; 具有法呢基转移酶抑制活性; 其制剂，含有它们的组合物及其作为药物的用途。

5. 发明申请

WO1994010164A1 4-QUINOLINYL DERIVATIVES WITH ANTI-HELICOBACTER ACTIVITY 审中-公开
标题翻译：具有抗真菌活性的4-喹啉衍生物
公开(公告)号：WO1994010164A1
公开(公告)日：1994-05-11
申请号：PCT/EP1993002884
申请日：1993-10-19
申请人： JANSSEN PHARMACEUTICA N.V. , VENET, Marc, Gaston , GUILLEMONT, Jérôme, Emiles, Georges , VERNIER, Daniel, Franck, Jean , ODDS, Franck, Christopher
发明人： JANSSEN PHARMACEUTICA N.V.
IPC分类号： C07D401/06
CPC分类号： C07D249/08 , C07D231/12 , C07D233/56 , C07D401/06
摘要： The present invention is concerned with novel quinoline derivatives having anti-Helicobacter activity of formula (I), the pharmaceutically acceptable acid addition salts therof, the stereochemically isomeric forms thereof, the quaternized forms thereof and the N &cir& _-oxides thereof, wherein -A- represents a bivalent radical of formula: (a) -N=CH-CH=CH-, (b) -CH=N-CH=CH-, (c) -N=N-CH=CH-, (d) -N=CH-N=CH-, (e) -N=CH-CH=N-, (f) -CH=N-N=CH-, (g) -N=N-N=CH-, (h) -N=N-CH=N-, or (i) -CH=CH-CH=CH-; R , R , R , R , R , R and R each independently represent hydrogen, halo, hydroxy, C1-4alkyloxy, C1-4alkyl, trifluromethyl, amino, mono- or di(C1-4alkyl)- amio or nitro, provided that when one substituent on a phenyl group is a nitro then the other substituents on said phenyl group are other than nitro; novel compositions comprising said compunds, processes of preparing said compounds and compositions and methods for treating subjects suffering from disorders or afflictions associated with Helicobacter infection.
摘要翻译：本发明涉及具有式（I）的抗幽门螺杆菌活性的新型喹啉衍生物，其药学上可接受的酸加成盐，其立体化学异构形式，其季铵化形式及其N-氧化物，其中-A - 表示式（a）-N = CH-CH = CH-，（b）-CH = N-CH = CH-，（c）-N = N-CH = CH-的二价基团，（d） -N = CH-N = CH-，（e）-N = CH-CH = N-，（f）-CH = NN = CH-，（g）-N = NN = CH-，（h）-N = N-CH = N-，或（i）-CH = CH-CH = CH-; R 1，R 2，R 3，R 4，R 5，R 6和R 7各自独立地表示氢，卤素，羟基，C 1-4烷氧基，C 1-4烷基，三氟甲基，氨基，单 - 或二（C 1-4烷基） - 氨基或硝基，条件是当苯基上的一个取代基为硝基时，所述苯基上的其它取代基不是硝基; 包含所述组合物的新型组合物，制备所述化合物的方法和组合物以及治疗患有与幽门螺杆菌感染相关的病症或苦难的受试者的方法。

6. 发明申请

WO1995022541A1 ENANTIOMERICALLY PURE(-)-LIAROZOLE 审中-公开
标题翻译：（ - ） - LIAROZOLE
公开(公告)号：WO1995022541A1
公开(公告)日：1995-08-24
申请号：PCT/EP1995000491
申请日：1995-02-10
申请人： JANSSEN PHARMACEUTICA N.V. , VENET, Marc, Gaston
发明人： JANSSEN PHARMACEUTICA N.V.
IPC分类号： C07D403/06
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08
摘要： This invention relates to the novel enantiomerically pure laevorotatory isomer of liarozole of formula (I) and the pharmaceutically acceptable acid addition salt forms thereof. These compounds are particularly useful in treating disorders which are characterized by an increased proliferation and/or abnormal differentiation of normal, preneoplastic or neoplastic epithelial cells. The compounds of formula (I) are particularly useful in the field of oncology. Also disclosed are compositions containing said novel compounds, methods of preparing said novel compounds as well as methods of using the mentioned compounds to treat the mentioned disorders.
摘要翻译：本发明涉及式（I）的噻唑并且其药学上可接受的酸加成盐形式的新型对映异构体纯的左旋异构体。这些化合物特别可用于治疗以正常，肿瘤前或肿瘤上皮细胞增殖和/或异常分化增加为特征的疾病。式（I）化合物在肿瘤学领域特别有用。还公开了含有所述新化合物的组合物，制备所述新化合物的方法以及使用所述化合物治疗所述疾病的方法。

7. 发明申请

WO1995022540A1 ENANTIOMERICALLY PURE (+)-LIAROZOLE 审中-公开
标题翻译：纯化（+） - 锂离子
公开(公告)号：WO1995022540A1
公开(公告)日：1995-08-24
申请号：PCT/EP1995000490
申请日：1995-02-10
申请人： JANSSEN PHARMACEUTICA N.V. , VENET, Marc, Gaston
发明人： JANSSEN PHARMACEUTICA N.V.
IPC分类号： C07D403/06
CPC分类号： C07D249/08 , C07D231/12 , C07D233/56
摘要： This invention relates to the novel enantiomerically pure dextrorotatory isomer of liarozole of formula (I) and the pharmaceutically acceptable acid addition salt forms thereof. These compounds are particularly useful in treating disorders which are characterized by an increased proliferation and/or abnormal differentiation of normal, preneoplastic or neoplastic epithelial cells. These compounds are particularly useful in the field of dermatology. Also disclosed are compositions containing said novel compounds, methods of preparing said novel compounds as well as methods of using the mentioned compounds to treat the mentioned disorders.
摘要翻译：本发明涉及式（I）的噻唑并且其药学上可接受的酸加成盐形式的新颖的对映体纯的右旋异构体。这些化合物特别可用于治疗以正常，肿瘤前或肿瘤上皮细胞增殖和/或异常分化增加为特征的疾病。这些化合物在皮肤病领域特别有用。还公开了含有所述新化合物的组合物，制备所述新化合物的方法以及使用所述化合物治疗所述疾病的方法。

8. 发明申请

WO1994011364A1 PROCESS FOR PREPARING ENANTIOMERICALLY PURE 6-[(4-CHLOROPHENYL)(1H_-TRIAZOL-1,2,4-TRIAZOL-1-YL)METHYL]-1-METHYL-1H_-BENZOTRIAZOLE 审中-公开
标题翻译：制备纯度6 - [（4-氯苯基）（1H，c] _-三唑-1,2,4-三唑-1-基]甲基] -1-甲基-1H-苯并噻唑的方法
公开(公告)号：WO1994011364A1
公开(公告)日：1994-05-26
申请号：PCT/EP1993003066
申请日：1993-11-02
申请人： JANSSEN PHARMACEUTICA N.V. , WILLEMSENS, Albert, Louis, Anna , VERSTAPPEN, Walter, Louis, Antoine , COPMANS, Alex, Herman , VANDENDRIESSCHE, Anna, Maria, Jozefa , DE KNAEP, Alfons, Gaston, Maria , VENET, Marc, Gaston
发明人： JANSSEN PHARMACEUTICA N.V.
IPC分类号： C07D403/06
CPC分类号： C07D249/08 , C07D231/12 , C07D233/56 , C07D249/18
摘要： A process for preparing (+)-6-[(4-chlorophenyl)(1H &cir& _-1,2,4-triazol-1-yl)methyl]-1-methyl-1H &cir& _-benzotriazole comprising the resolution of (+/-)-6-[(4-chlorophenyl-hydrazinomethyl)-1-methyl-1H &cir& _-benzotriazole and converting the appropriate enantiomerically pure hydrazine intermediate into (+)-6-[(4-chlorophenyl)(1H &cir& _-1,2,4-triazol-1-yl)methyl]-1-methyl-1H &cir& _-benzotriazole.
摘要翻译：制备（+） - 6 - [（4-氯苯基）（1H，c'，1,2,4-三唑-1-基）甲基] -1-甲基-1H-苯并三唑的方法，包括（ +/-） - 6 - [（4-氯苯基 - 肼基甲基）-1-甲基-1H-苯并三唑，并将适当的对映体纯肼中间体转化为（+） - 6 - [（4-氯苯基）（1H， -1,2,4-三唑-1-基）甲基] -1-甲基-1H-苯并三唑。

9. 发明申请

WO1997034897A1 FUSED IMIDAZOLE DERIVATIVES AS MULTIDRUG RESISTANCE MODULATORS 审中-公开
标题翻译：作为多电阻电阻调节剂的熔融咪唑衍生物
公开(公告)号：WO1997034897A1
公开(公告)日：1997-09-25
申请号：PCT/EP1997001264
申请日：1997-03-11
申请人： JANSSEN PHARMACEUTICA N.V. , JANSSENS, Frans, Eduard , LEENAERTS, Joseph, Elisabeth , SOMMEN, François, Maria , SURLERAUX, Dominique, Louis, Nestor, Ghislaine
发明人： JANSSEN PHARMACEUTICA N.V.
IPC分类号： C07D487/04
CPC分类号： C07D487/14 , C07D471/04 , C07D487/04 , C07D495/14
摘要： This invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein the dotted line is an optional bond; n is 1 or 2; R is hydrogen; halo; formyl; C1-4alkyl optionally substituted with hydroxy, C1-4alkyloxy, C1-4alkylcarbonyloxy, imidazolyl, thiazolyl or oxazolyl; or a radical of formula -X-COOR , -X-CONR R or -X-COR wherein -X- is a direct bond, C1-4alkanediyl or C2-6alkenediyl; R is hydrogen, C1-12alkyl, Ar, Het, C1-6alkyl substituted with C1-4alkyloxy, aryl or heteroaryl; R and R each independently are hydrogen or C1-4alkyl; R is hydrogen, halo, C1-4alkyl, hydroxyC1-4alkyl, C1-4alkyloxycarbonyl, carboxyl, formyl or phenyl; R is hydrogen, C1-4alkyl or C1-4alkyloxy; R is hydrogen, halo, C1-4alkyl, C1-4alkyloxy or haloC1-4alkyl; Z is -CH2-, -CH2-CH2-, -CH=CH-, -CHOH-CH2-, -O-CH2-, -C(=O)-CH2- or -C(=NOH)-CH2-; -A-B- is a bivalent radical; A is a direct bond, optionally substituted C1-6alkanediyl, C1-6alkanediyl-oxy-C1-6alkanediyl, carbonyl, C1-6alkanediylcarbonyl, optionally substituted C1-6alkanediyloxy; A is a direct bond or C1-6alkanediyl; and Q is aryl. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for inhibiting or reversing the effects of multidrug resistance.
摘要翻译：本发明涉及式（I）化合物，N-氧化物形式，其药学上可接受的加成盐和立体化学异构形式，其中虚线是任选的键; n为1或2; R 1是氢; 光环; 甲酰基; 任选被羟基，C 1-4烷氧基，C 1-4烷基羰基氧基，咪唑基，噻唑基或恶唑基取代的C 1-4烷基; 或式-X-COOR 5，-X-CONR 6 R 7或-X-COR 10基团，其中-X-是直接键，C 1-4烷二基或C 2-6亚烯基; R 5是氢，C 1-12烷基，Ar，Het，被C 1-4烷氧基，芳基或杂芳基取代的C 1-6烷基; R 6和R 7各自独立地为氢或C 1-4烷基; R 2是氢，卤素，C 1-4烷基，羟基C 1-4烷基，C 1-4烷氧基羰基，羧基，甲酰基或苯基; R 3是氢，C 1-4烷基或C 1-4烷氧基; R 4是氢，卤素，C 1-4烷基，C 1-4烷氧基或卤代C 1-4烷基; Z是-CH 2 - ， - CH 2 -CH 2 - ， - CH = CH-，-CHOH-CH 2 - ， - O-CH 2 - ， - C（= O）-CH 2 - 或-C（= NOH） -A-B-是二价基团; A 1是直接键，任选取代的C 1-6烷二基，C 1-6烷二基 - 氧基-C 1-6烷二基，羰基，C 1-6烷二基羰基，任选取代的C 1-6烷二基氧基; A 2是直接键或C 1-6烷二基; Q为芳基。公开了用于制备所述产品的方法，包含所述产品的制剂及其作为药物的用途，特别是用于抑制或逆转多药耐药性的作用。

10. 发明申请

WO1996033193A1 NOVEL TRIAZOLONES AS APOLIPOPROTEIN-B SYNTHESIS INHIBITORS 审中-公开
标题翻译：新型三唑酮作为APOLIPOPROTEIN-B合成抑制剂
公开(公告)号：WO1996033193A1
公开(公告)日：1996-10-24
申请号：PCT/EP1996001585
申请日：1996-04-12
申请人： JANSSEN PHARMACEUTICA N.V. , HEERES, Jan , BACKX, Leo, Jacobus, Jozef , LUYTS, Paul, August, Clement , DE CHAFFOY DE COURCELLES, Didier, Robert, Guy, Gabriël
发明人： JANSSEN PHARMACEUTICA N.V.
IPC分类号： C07D405/14
CPC分类号： C07D249/08 , C07D231/12 , C07D233/56
摘要： The present invention concerns novel compounds of formula (I), wherein R is C1-10alkyl, C3-7cycloalkyl or C1-6alkyl substituted with C3-7cycloalkyl; R is hydrogen or C1-6alkyl; Alk represents C1-3alkanediyl; -A- represents a bivalent radical of the formula: (a) -CH=CH-N=CH-, (b) -N=CH-N=CH-, (c) -CH=N-N=CH-, (d) -CH=CH-CH=N-; in said bivalent radicals a hydrogen atom may be replaced by C1-6alkyl; and Ar is unsubstituted phenyl; phenyl substituted with up to two substituents selected from halo, C1-6alkyl or C1-6alkyloxy; unsubstituted naphthyl; or naphthyl substituted with up to two substituents selected from halo, C1-6alkyl or C1-6alkyloxy; the stereochemically isomeric forms thereof, and the pharmaceutically acceptable acid addition salts thereof. The present invention further comprises the pharmaceutical compositions comprising compounds of formula (I), the preparation thereof as well as the use as a medicine in the treatment of hyperlipidemia.
摘要翻译：本发明涉及新的式（I）化合物，其中R 1是C 1-10烷基，C 3-7环烷基或被C 3-7环烷基取代的C 1-6烷基; R 2是氢或C 1-6烷基; Alk表示C1-3烷二基; -A-表示下式的二价基团：（a）-CH = CH-N = CH-，（b）-N = CH-N = CH-，（c）-CH = NN = CH-，（d ）-CH = CH-CH = N-; 在所述二价基团中，氢原子可被C 1-6烷基取代; 和Ar是未取代的苯基; 被至多两个选自卤素，C 1-6烷基或C 1-6烷氧基的取代基取代的苯基; 未取代的萘基; 或被至多两个选自卤素，C 1-6烷基或C 1-6烷氧基的取代基取代的萘基; 其立体化学异构形式及其药学上可接受的酸加成盐。本发明还包含包含式（I）化合物，其制备方法以及用作治疗高脂血症药物的药物组合物。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式